Anti-hyperlipidemic Activity of Thieno - [2, 3-d] - Pyrimidin-4-(3H)-ones

Abstract

Aim: The present study was aimed to evaluate some newly synthesized thieno -[2, 3-d] -pyrimidin-4-(3H)-ones namely SR-C1 to SR-C12 for their anti-hyperlipidemic activity. Materials and Methods:Anti-hyperlipidemic activity was evaluated using Triton 1339-induced hyperlipedemia in rats as an experimental model. Plasma triglycerides, total cholesterol, HDL-C, LDL-C, atherogenic index (AI) and LDL-C/HDL-C ratio were determined to assess the anti-hyperlipidemic activity.Results: SR-C1,SR-C4, SR-C5, SR-C6, SR-C7, SR-C11 and SR-C12 have shown significant antihyperlipidemic activity by decreasing the total cholesterol and triglyceride, LDL-cholesterol, atherogenic index and LDL/HDL ratio (p < 0.001) and by increasing the HDL-Cholesterol (p < 0.001). Conclusion:The findings of the present study clearly demonstrates that methyl, methoxy, chloro, dimethylamino, dimethoxy and trimethoxy functional groups possess cholesterol-suppressive capacities and has an ability to attenuate the accelerated development of atherosclerosis in hypercholesterolemic models. However, hydroxyl and nitro derivatives did not show any hypolipidemic activity.

Antihyperlipidemic effect of selected pyrimidine derivatives mediated through multiple pathways

“…Oxidative stress markers such as GST, GSH, and catalase could reflect production of free radicals and defense against formation of ROS under the oxidative stress [32]. Groups treated with SR-5, SR-8, SR-9, SR-10, and simvastatin prevented oxidative stress and restored tissue antioxidants (Figure 3) to treat hyperlipidemia which is in agreement with previous studies regarding selected pyrimidine class [33]. Our data suggest that the antioxidative activities of compounds are also crucial to their hepatoprotective and antihyperlipidemic effect [34].…”